Tag: 100-200

Efficient access to 5-substituted thiazoles by a novel metallotropic rearrangement was written by Zambon, Alfonso;Borsato, Giuseppe;Brussolo, Stefania;Frascella, Pietrogiulio;Lucchini, Vittorio. And the article was included in Tetrahedron Letters in 2008.COA of Formula: C9H7NS This article mentions the following:

A novel rearrangement process involving the migration of trimethylstannanyl or trimethylsilanyl groups around the thiazole ring provides access to either 2- or 5-metalated thiazoles by tuning the reaction conditions. The proposed mechanism, based on exptl. evidence, is characterized by the catalytic role of thiazole bisadducts as metal-transfer agents. In the experiment, the researchers used many compounds, for example, 5-Phenylthiazole (cas: 1826-13-7COA of Formula: C9H7NS).

5-Phenylthiazole (cas: 1826-13-7) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.COA of Formula: C9H7NS

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Dehydration Polymerization for Poly(hetero)arene Conjugated Polymers was written by Mirabal, Rafael A.;Vanderzwet, Luke;Abuadas, Sara;Emmett, Michael R.;Schipper, Derek. And the article was included in Chemistry – A European Journal in 2018.SDS of cas: 1826-13-7 This article mentions the following:

The lack of scalable and sustainable methods to prepare conjugated polymers belies their importance in many enabling technologies. Accessing high-performance poly(hetero)arene conjugated polymers by dehydration has remained an unsolved problem in synthetic chem. and has historically required transitional-metal coupling reactions. Herein, we report a dehydration method that allows access to conjugated heterocyclic materials. By using the technique, we have prepared a series of small mols. and polymers. The reaction avoids using transition metals, proceeds at room temperature, the only required reactant is a simple base and water is the sole byproduct. The dehydration reaction is tech. simple and provides a sustainable and straightforward method to prepare conjugated heteroarene motifs. In the experiment, the researchers used many compounds, for example, 5-Phenylthiazole (cas: 1826-13-7SDS of cas: 1826-13-7).

5-Phenylthiazole (cas: 1826-13-7) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.SDS of cas: 1826-13-7

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Discovery of BPR1R024, an Orally Active and Selective CSF1R Inhibitor that Exhibits Antitumor and Immunomodulatory Activity in a Murine Colon Tumor Model was written by Lee, Kun-Hung;Yen, Wan-Ching;Lin, Wen-Hsing;Wang, Pei-Chen;Lai, You-Liang;Su, Yu-Chieh;Chang, Chun-Yu;Wu, Cai-Syuan;Huang, Yu-Chen;Yang, Chen-Ming;Chou, Ling-Hui;Yeh, Teng-Kuang;Chen, Chiung-Tong;Shih, Chuan;Hsieh, Hsing-Pang. And the article was included in Journal of Medicinal Chemistry in 2021.HPLC of Formula: 55661-33-1 This article mentions the following:

Colony-stimulating factor-1 receptor (CSF1R) is implicated in tumor-associated macrophage (TAM) repolarization and has emerged as a promising target for cancer immunotherapy. Herein, we describe the discovery of orally active and selective CSF1R inhibitors by property-driven optimization of BPR1K871 (9), our clin. multitargeting kinase inhibitor. Mol. docking revealed an addnl. nonclassical hydrogen-bonding (NCHB) interaction between the unique 7-aminoquinazoline scaffold and the CSF1R hinge region, contributing to CSF1R potency enhancement. Structural studies of CSF1R and Aurora kinase B (AURB) demonstrated the differences in their back pockets, which inspired the use of a chain extension strategy to diminish the AURA/B activities. A lead compound BPR1R024 (12) exhibited potent CSF1R activity (IC₅₀ = 0.53 nM) and specifically inhibited protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth. In vivo, oral administration of 12 mesylate delayed the MC38 murine colon tumor growth and reversed the immunosuppressive tumor microenvironment with the increased M1/M2 ratio. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1HPLC of Formula: 55661-33-1).

Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.HPLC of Formula: 55661-33-1

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Synthesis of pyrazolo-enaminones, bipyrazoles and pyrazolopyrimidines and evaluation of antioxidant and antimicrobial properties was written by Akhramez, Soufiane;Oumessaoud, Asmaa;Hibot, Achraf;Talbi, Soumaya;Hamri, Salha;Ketatni, El Mostafa;Ouchetto, Hajiba;Hafid, Abderrafia;Ayad, Houda;El Abbadi, Noureddine;Zanane, Chorouk;Latrache, Hassan;Khouili, Mostafa;Pujol, Maria Dolors. And the article was included in Arabian Journal of Chemistry in 2022.Product Details of 55661-33-1 This article mentions the following:

A novel pyrazolo-enaminones I [R = C₆H₅, 3-Br-C₆H₄, 4-OCH₃-2-NO₂-C₆H₃, etc.], bipyrazoles II [R¹ = H, C₆H₅; R² = C₆H₅, 4-CH₃C₆H₄, 4-NO₂C₆H₄, 2,4-NO₂C₆H₃] and pyrazolopyridines e.g., III from 1-(5-hydroxy-3-methyl-1-phenyl-1H-pyrazol-4-yl)butane-1,3-dione and 4-methyl-2-phenyl-2H-pyrazolo[3,4-b]pyridine-3,6(3aH,7H)-dione was synthesized by assisted heating with microwave radiation without any catalyst. The pyridine and pyrazole ring formation had been developed from easily accessible enamino keto esters by formylation followed by intramol. cyclization. The general applicability for the synthesis of the important pyrazolo-enaminones, bipyrazoles and pyrazolo-pyridines heterocycles was attributed to simplicity of operation, synthesis without catalyst, energy efficiency (shorter reaction time under microwave irradiation), good yields, more environmentally friendly and more cost-effective procedure. The antioxidant activity and antibacterial activity of new heterocyclic compounds was evaluated by free radical scavenging by DPPH assay. Several of these compounds showed good activity against both Gram-pos. (S. aureus) and Gram-neg. (E. coli) bacteria. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Product Details of 55661-33-1).

Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Product Details of 55661-33-1

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Photoinduced Heterogeneous C-H Arylation by a Reusable Hybrid Copper Catalyst was written by Choi, Isaac;Mueller, Valentin;Lole, Gaurav;Koehler, Robert;Karius, Volker;Vioel, Wolfgang;Jooss, Christian;Ackermann, Lutz. And the article was included in Chemistry – A European Journal in 2020.Recommanded Product: 5-Phenylthiazole This article mentions the following:

Heterogeneous copper catalysis enabled photoinduced C-H arylations of heteroarenes with aryl halides under exceedingly mild conditions at room temperature to afford aryl heteroarenes such as I [R = H, 6-OMe, 5-Cl, etc.; Ar = Ph, 4-MeC₆H₄, 2-MeOC₆H₄, etc.; X = O, S, NMe]. The hybrid copper catalyst could be reused without significant loss of catalytic efficacy. Detailed studies in terms of TEM, HRTEM and XPS anal. of the hybrid copper catalyst, among others, supported its outstanding stability and reusability. In the experiment, the researchers used many compounds, for example, 5-Phenylthiazole (cas: 1826-13-7Recommanded Product: 5-Phenylthiazole).

5-Phenylthiazole (cas: 1826-13-7) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Recommanded Product: 5-Phenylthiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Synthesis and biological evaluation of novel trichodermin derivatives as antifungal agents was written by Zheng, Min;Yao, Ting-Ting;Xu, Xiao-Jun;Cheng, Jing-Li;Zhao, Jin-Hao;Zhu, Guo-Nian. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2014.Safety of 2-Methylthiazol-5-amine This article mentions the following:

To discover more potential antifungal agents, 17 novel trichodermin derivatives were designed and synthesized. The structures of all the synthesized compounds were confirmed by ¹H NMR, ESI-MS and HRMS. Their antifungal activities against Ustilaginoidea oryzae and Pyricularia oryzae were evaluated. Most of the target compounds showed potent inhibitory activity, in which I showed superior inhibitory effects than the parent compound and com. fungicide prochloraz. Addnl., compound II was found to be active against all tested fungal strains, with EC₅₀ values of 0.47 and 3.71 mg L^-1, resp. In the experiment, the researchers used many compounds, for example, 2-Methylthiazol-5-amine (cas: 89281-44-7Safety of 2-Methylthiazol-5-amine).

2-Methylthiazol-5-amine (cas: 89281-44-7) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Safety of 2-Methylthiazol-5-amine

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Structure-Guided Rescaffolding of Selective Antagonists of BCL-X_L was written by Koehler, Michael F. T.;Bergeron, Philippe;Choo, Edna F.;Lau, Kevin;Ndubaku, Chudi;Dudley, Danette;Gibbons, Paul;Sleebs, Brad E.;Rye, Carl S.;Nikolakopoulos, George;Bui, Chinh;Kulasegaram, Sanji;Kersten, Wilhelmus J. A.;Smith, Brian J.;Czabotar, Peter E.;Colman, Peter M.;Huang, David C. S.;Baell, Jonathan B.;Watson, Keith G.;Hasvold, Lisa;Tao, Zhi-Fu;Wang, Le;Souers, Andrew J.;Elmore, Steven W.;Flygare, John A.;Fairbrother, Wayne J.;Lessene, Guillaume. And the article was included in ACS Medicinal Chemistry Letters in 2014.Computed Properties of C5H4ClNO2S This article mentions the following:

Because of the promise of BCL-2 antagonists in combating chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL), interest in addnl. selective antagonists of antiapoptotic proteins has grown. Beginning with a series of selective, potent BCL-X_L antagonists containing an undesirable hydrazone functionality, in silico design and X-ray crystallog. were utilized to develop alternative scaffolds that retained the selectivity and potency of the starting compounds In the experiment, the researchers used many compounds, for example, Methyl2-chloro-4-thiazolecarboxylate (cas: 850429-61-7Computed Properties of C5H4ClNO2S).

Methyl2-chloro-4-thiazolecarboxylate (cas: 850429-61-7) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Computed Properties of C5H4ClNO2S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Benzimidazole-carboxamides as potent and bioavailable stearoyl-CoA desaturase (SCD1) inhibitors from ligand-based virtual screening and chemical optimization was written by Matter, Hans;Zoller, Gerhard;Herling, Andreas W.;Sanchez-Arias, Juan-Antonio;Philippo, Christophe;Namane, Claudie;Kohlmann, Markus;Pfenninger, Anja;Voss, Marc D.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2013.SDS of cas: 55661-33-1 This article mentions the following:

The discovery of potent benzimidazole stearoyl-CoA desaturase (SCD1) inhibitors by ligand-based virtual screening is described. ROCS 3D-searching gave a favorable chem. motif that was subsequently optimized to arrive at a chem. series of potent and promising SCD1 inhibitors. In particular, compound SAR224 was selected for further pharmacol. profiling based on favorable in vitro data. After oral administration to male ZDF rats, this compound significantly decreased the serum fatty acid desaturation index, thus providing conclusive evidence for SCD1 inhibition in vivo by SAR224. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1SDS of cas: 55661-33-1).

Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.SDS of cas: 55661-33-1

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Novel 2-(4-methylsulfonylphenyl)pyrimidine derivatives as highly potent and specific COX-2 inhibitors was written by Orjales, Aurelio;Mosquera, Ramon;Lopez, Beatriz;Olivera, Roberto;Labeaga, Luis;Nunez, M. Teresa. And the article was included in Bioorganic & Medicinal Chemistry in 2008.COA of Formula: C4H6N2S This article mentions the following:

New series of 2-(4-methylsulfonylphenyl) and 2-(4-sulfamoylphenyl)pyrimidines were synthesized and evaluated for their ability to inhibit cyclooxygenase-2 (COX-2). COX-1 and COX-2 inhibitory activity of these compounds was determined using purified enzyme (PE) and human whole blood (HWB) assays. Extensive structure-activity relationship (SAR) work was carried out within these series, and a wide number of potent and specific COX-2 inhibitors were identified (HWB COX-2 IC₅₀ = 2.4-0.3 nM and 80- to 780-fold more selective than rofecoxib). In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1COA of Formula: C4H6N2S).

Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.COA of Formula: C4H6N2S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

CNDO/S method interpretation of ultraviolet spectra of phenylthiazoles was written by Bouscasse, L.;Lebreton, M.;Aune, J. P.. And the article was included in Spectroscopy Letters in 1994.Application of 1826-13-7 This article mentions the following:

The UV spectra of three phenylthiazoles are reported. These exptl. results are interpreted using CNDO/S method (CNDO for Spectroscopy). Calculations show that the observed transitions, except two, are pseudo π → π^* type transitions. In the experiment, the researchers used many compounds, for example, 5-Phenylthiazole (cas: 1826-13-7Application of 1826-13-7).

5-Phenylthiazole (cas: 1826-13-7) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Application of 1826-13-7

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica